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■ Synthesis and Evaluation of Diaminopyrimidine Derivatives as Dual Inhibitors of EGFR and SRC for Antitumor Treatment

Longjia Yan,* Yi Le, Dongmei Chen, Yumei Chen, Di Zhang, and Lan Yang

*School of Pharmaceutical Sciences, Guizhou University, 440 Chongyi Building,Guizhou University, Huaxi District, China

Abstract

In this paper, a series of novel diaminopyrimidine derivatives was designed and synthesized using palladium-catalyzed Buchwald–Hartwig-type heteroarylamination procedure. And then, they were evaluated for antitumor activity in vitro on wild type epidermal growth factor receptor tyrosine kinase (EGFRwt-TK), c-Src and four human cancer cell lines including A549, PC-3, SMMC-7721 and K562. The results displayed that some of the compounds had good activities. Especially 2-(2-cycloheptylamino-5-trifluoromethylpyrimidin-4-ylamino)-N-methylbenzami-de (1h) showed high antitumor activities against four cancer cell lines with 2.33, 7.46, 1.13 and 1.28 μM. Furthermore, the IC50 values of compound 1h for EGFR and Src reached in 0.86 μM and 0.22 μM.